Structure–activity relationships of SERMs optimized for uterine antagonism and ovarian safety

Structure–activity relationship studies are described, which led to the discovery of novel selective estrogen receptor modulators (SERMs) for the potential treatment of uterine fibroids. The SAR studies focused on limiting brain exposure and were guided by computational properties. Compounds with limited impact on the HPO axis were selected using serum estrogen levels as a biomarker for ovarian stimulation.

SAR studies are described, which led to the discovery of novel SERMs for the treatment of uterine fibroids.Figure optionsDownload as PowerPoint slide